- Piperine derivative as well as preparation method and application thereof
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The invention provides a piperine derivative as well as a preparation method and an application thereof. The piperine derivative is a compound shown as a formula (I), or a salt thereof, or a stereoisomer thereof, or a hydrate thereof. The compound provided by the invention can effectively protect nerve cells and improve the survival rate of the nerve cells, so that the compound provided by the invention can effectively treat neurodegenerative diseases and can be used for preparing medicines for treating the neurodegenerative diseases.
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Paragraph 0142; 0263-0265
(2020/05/08)
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- Identification and optimization of piperine analogues as neuroprotective agents for the treatment of Parkinson's disease via the activation of Nrf2/keap1 pathway
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Parkinson's disease (PD) is a slowly progressive and complex neurodegenerative disorder. Up to date, there are no approved drugs that could slow or reverse the neurodegenerative process of PD. Here, we reported the synthesis of series of piperine analogues and the evaluation of their neuroprotective effects against hydrogen peroxide (H2O2) induced damage in the neuron-like PC12 cells. Among these analogues, 3b exhibited the most potent protection effect and its underlying mechanism was further investigated. Further results indicated that the ROS scavenging and cytoprotection effect of 3b might be related to the Nrf2 activation and upregulation of related phase II antioxidant enzymes, such as HO-1 and NQO1. In in vivo study, oral administration (100 mg/kg) of 3b significantly attenuated PD-associated behavioral deficits in a 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced mouse model of PD and protected tyrosine hydroxylase-immunopositive dopaminergic neurons. Our results provided evidence that 3b might be a promising candidate for Parkinson's disease treatment.
- Cai, Xiaoying,Chen, Lijuan,Hong, Feng,Kuang, Shuang,Li, Yan,Ma, Xu,Qi, Wenyan,Shi, Mingsong,Wang, Lun,Xu, Ruiling,Xue, Linlin,Ye, Haoyu,Zhang, Ruijia
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- Indium-mediated microwave-assisted one-pot synthesis of α,β-unsaturated amides
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A stereoselective synthesis of α,β-unsaturated-N,N-diethyl amides was achieved by a one-pot reaction of triphenylphosphine, an aromatic aldehyde, and N,N-diethyl chloroacetamide in the presence of indium under microwave-assisted and solvent-free condition.
- Feng, Sunlin,Jiang, Shilei,Zhang, Zhiying,Yu, Xiaochun
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experimental part
p. 392 - 394
(2010/11/18)
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- Synthesis of α β,-unsaturated amide via phosphonium ylide
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A series of ,-unsaturated amides were prepared by the Wittig reaction of N,N-diethylamidemethylenetriphenylphosphorane ylide with aldehydes with moderate to good yields. Copyright Taylor & Francis Group, LLC.
- Jiang, Shilei,Yang, Kefeng,Yu, Xiaochun
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supporting information; experimental part
p. 1759 - 1767
(2009/11/30)
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- Microwave-assisted one-pot synthesis of α, β-unsaturated amides under solvent-free conditions
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Under microwave-assisted solvent-free conditions a one-pot reaction of triphenylphosphine, an aldehyde and N, N-diethyl chloroacetamide in the presence of zinc dust affords α, β-unsaturated amides stereoselectively in good yield. In comparison with the co
- Jiang, Shilei,Xie, Yuanyuan,Yu, Xiaochun
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experimental part
p. 24 - 26
(2009/10/02)
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